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大鼠输精管中缺乏ε-阿片受体的证据。

Lack of evidence for epsilon-opioid receptors in the rat vas deferens.

作者信息

Sheehan M J, Hayes A G, Tyers M B

机构信息

Department of Neuropharmacology, Glaxo Group Research Ltd., Ware, Hertfordshire, U.K.

出版信息

Eur J Pharmacol. 1988 Sep 23;154(3):237-45. doi: 10.1016/0014-2999(88)90197-5.

Abstract

Experiments were performed to test the hypothesis that the field-stimulated rat vas deferens preparation contains opioid receptors, other than of mu-type, which mediate part of the inhibitory effect of beta-endorphin. The Piebald Viral Glaxo strain of rats was used. The reported finding that delta-opioid receptors are present in Sprague-Dawley rat vas deferens, the effects of which are greatly enhanced in reduced calcium concentrations, could not be replicated in the rat strain used. Reducing the calcium concentration from 2.5 to 1.25 mM improved the response to opioid drugs: all full agonists were about 10 times more potent, the partial agonist normorphine became able to inhibit the twitch completely, and morphine (which behaves as a competitive antagonist in 2.5 mM Ca2+) appeared to behave as a partial agonist. The pA2 values for antagonism by naloxone in low calcium of the mu-selective peptide [D-Ala2,MePhe4,Gly(ol)5]enkephalin and other mu- or delta-selective agonists were consistent with an action at mu-receptors only. The value for beta-endorphin was slightly but significantly lower. A similar small discrepancy was found with two other competitive antagonists. The discrepancy remained in the presence of the peptidase inhibitors thiorphan, bestatin and bacitracin. Responses to both [D-Ala2,MePhe4,Gly(ol)5]enkephalin and beta-endorphin were attenuated by the irreversible antagonists beta-funaltrexamine and beta-chlornaltrexamine.(ABSTRACT TRUNCATED AT 250 WORDS)

摘要

进行实验以检验以下假设

电场刺激的大鼠输精管制剂中存在除μ型以外的阿片受体,这些受体介导了β-内啡肽的部分抑制作用。使用的是斑驳病毒葛兰素株大鼠。已报道在Sprague-Dawley大鼠输精管中存在δ-阿片受体,在钙浓度降低时其作用会大大增强,但在所用的大鼠品系中无法重复这一发现。将钙浓度从2.5 mM降至1.25 mM可改善对阿片类药物的反应:所有完全激动剂的效力提高约10倍,部分激动剂去甲吗啡能够完全抑制抽搐,而吗啡(在2.5 mM Ca2+中表现为竞争性拮抗剂)似乎表现为部分激动剂。纳洛酮在低钙条件下对μ选择性肽[D-Ala2,MePhe4,Gly(ol)5]脑啡肽和其他μ或δ选择性激动剂的拮抗作用的pA2值仅与对μ受体的作用一致。β-内啡肽的值略低但有显著差异。在另外两种竞争性拮抗剂中也发现了类似的小差异。在肽酶抑制剂硫醇苯丙氨酸、贝司他汀和杆菌肽存在的情况下,差异仍然存在。对[D-Ala2,MePhe4,Gly(ol)5]脑啡肽和β-内啡肽的反应均被不可逆拮抗剂β-氟诺啡烷和β-氯诺啡烷减弱。(摘要截断于250字)

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